| Identification | Back Directory | [Name]
Olutasidenib (Synonyms: FT-2102) | [CAS]
1887014-12-1 | [Synonyms]
FT-2102
OLUTASIDENIB
Olutasidenib (FT-2102)
Olutasidenib (Synonyms: FT-2102)
5-[[(1S)-1-(6-Chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino]-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile
2-Pyridinecarbonitrile, 5-[[(1S)-1-(6-chloro-1,2-dihydro-2-oxo-3-quinolinyl)ethyl]amino]-1,6-dihydro-1-methyl-6-oxo- | [Molecular Formula]
C18H15ClN4O2 | [MOL File]
1887014-12-1.mol | [Molecular Weight]
354.79 |
| Chemical Properties | Back Directory | [Boiling point ]
603.3±55.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A crystalline solid | [pka]
10.44±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) [1][2]. | [in vivo]
Olutasidenib (FT-2102, three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals) exhibits potent anti-tumor activity in HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice[2]. | Animal Model: | HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice[2]. | | Dosage: | 12.5, 25, and 50 mg/kg. | | Administration: | Three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals. | | Result: | Showed a time and dose-dependent inhibition of 2-HG levels in in tumor.
At the highest dose tested in these studies (50 mg/kg), treatment with FT-2102 inhibited 2-HG levels in the tumor by >90% for up to 24 hours after the last dose in the HCT116-IDH1-R132H/+ xenograft model.
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| [IC 50]
IDH1 | [storage]
Store at -20°C | [References]
[1] JM Watts, et al. A phase 1 dose escalation study of the IDH1m inhibitor, FT-2102, in patients with acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS).
[2] Justin A. Caravella, et al. Structure-based design and identification of FT-2102 (olutasidenib), a potent mutant-selective IDH1 inhibitor. J Med Chem. 2020. |
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